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On the utility of coupling polarised light microscopy to a solubility assay in drug discovery†
P. A. MacFaul,A. J. Ratcliffe,M. Támara,S. Vernon
MedChemComm Pub Date : 04/08/2016 00:00:00 , DOI:10.1039/C6MD00138F
Abstract

Polarised light microscopy has been used to assess the physical form of over 800 compounds whose aqueous solubility has been measured in a solubility assay in a drug discovery setting. Analysis of the data indicates the presence of a wide range of physical forms although encouragingly many compounds do appear to be in a crystalline or semi-crystalline form. Approximately 15% of the compounds were identified as remaining in an amorphous state. For these compounds there is a high risk that the solubility value generated will be an over-estimate of the true solubility of the compound.

Graphical abstract: On the utility of coupling polarised light microscopy to a solubility assay in drug discovery
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